Benzolactam derivatives

Abstract

A benzolactam derivative represented by the following formula (I): ##STR1## wherein n represents an integer of from 1 to 3; R 1 represents a straight- or branched-chain alkyl group or an aralkyl group; R 2 represents a straight- or branched-chain alkyl group; R 3 and R 4 independently represent a hydrogen atom or a straight- or branched-chain alkyl group, and when R 3 and R 4 are adjacent each other on the phenyl group, they may be combined to form a cycloalkyl ring together with two carbon atoms of the phenyl group to which R 3 and R 4 bind, and said cycloalkyl ring may optionally have one or more substituents; and a anti-retroviral agent comprising the same as an active ingredient.

What is claimed is: 
     
       1. A benzolactam represented by the following formula (I): ##STR13## wherein n represents an integer of from 1 to 3; R 1  represents a straight- or branched-chain alkyl group having 1 to 12 carbon atoms or a benzyl group or a phenethyl group; R 2  represents a straight- or branched-chain alkyl group having 1 to 12 carbon atoms; R 3  and R 4  independently represent a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 12 carbon atoms, and when R 3  and R 4  are adjacent each other on the phenyl group, they may be combined to form a cycloalkyl ring having 5 to 7 carbon atoms together with 2 carbon atoms of the phenyl group to which R 3  and R 4  bind. 
     
     
       2. The benzolactam according to claim 1, wherein R 3  and R 4  form the cycloalkyl ring, and wherein the cycloalkyl ring is substituted with at least one lower alkyl group. 
     
     
       3. The benzolactam according to claim 1, wherein n is 1 or 2; R 1  represents a functional group selected from the group consisting of isopropyl group, isobutyl group, t-butyl group, n-octyl group, n-nonyl group, n-decanyl group, and benzyl group; R 2  represents a functional group selected from the group consisting of methyl group, n-octyl group, n-nonyl group, and n-decanyl group; and R 3  and R 4  independently represent a hydrogen atom or a straight- or branched-chain alkyl group containing 1 to 12 carbon atoms or they form a 6-membered cycloalkyl ring. 
     
     
       4. The benzolactam according to claim 3, wherein R 3  and R 4  form the 6-membered cycloalkyl ring, and wherein the cycloalkyl ring is substituted with at least one lower alkyl group. 
     
     
       5. The benzolactam according to claim 1, wherein R 1  represents a functional group selected from the group consisting of isopropyl group, isobutyl group, and t-butyl group; R 2  represents a methyl group; and R 3  and R 4  independently represent a hydrogen atom or a straight-chain alkyl group containing 10 carbon atoms or they form a 6-membered cycloalkyl ring. 
     
     
       6. The benzolactam according to claim 5, wherein R 3  and R 4  form the 6-membered cycloalkyl ring, and wherein the cycloalkyl ring is substituted with at least one methyl group. 
     
     
       7. An anti-retroviral agent comprising as an active ingredient a benzolactam represented by the following formula (I): ##STR14## wherein n represents an integer of from 1 to 3; R 1  represents a straight- or branched-chain alkyl group having 1 to 12 carbon atoms or a benzyl group or a phenethyl group; R 2  represents a straight- or branched-chain alkyl group having 1 to 12 carbon atoms; R 3  and R 4  independently represent a hydrogen atom or a straight- or branched-chain alkyl group having 1 to 12 carbon atoms, and when R 3  and R 4  are adjacent each other on the phenyl group, they may be combined to form a cycloalkyl ring having 5 to 7 carbon atoms together with 2 carbon atoms of the phenyl group to which R 3  and R 4  bind. 
     
     
       8. The anti-retroviral agent according to claim 7, wherein R 3  and R 4  are combined to form the cycloalkyl ring, and wherein the cycloalkyl ring has at least one lower alkyl group. 
     
     
       9. The anti-retroviral agent according to claim 7, wherein the retrovirus is a human acquired immunodeficiency virus.